5-(7-bromo-2,3-dihydro-benzo[1,4]dioxin-6-yl)-4-phenyl-thiazole-2-carboxylic acid ethyl ester | 721399-94-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并二恶烷
• 英文名称: 5-(7-bromo-2,3-dihydro-benzo[1,4]dioxin-6-yl)-4-phenyl-thiazole-2-carboxylic acid ethyl ester
• 英文别名: ethyl 5-(6-bromo-2,3-dihydro-1,4-benzodioxin-7-yl)-4-phenyl-1,3-thiazole-2-carboxylate
• CAS: 721399-94-6
• 化学式: C₂₀H₁₆BrNO₄S
• 分子量: 446.321
• InChiKey: RTGHJEFXTJLEQL-UHFFFAOYSA-N

物化性质

• 沸点：
  524.8±60.0 °C(Predicted)
• 密度：
  1.476±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  85.9
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] 4, 5-DIARYLTHIAZOLE DERIVATIVES AS CB-1 LIGANDS<br/>[FR] DERIVES DE 4, 5-DIARYLTHIAZOLE UTILISES EN TANT QUE LIGANDS DU CB-1
  申请人：ASTRAZENECA AB

  公开号：WO2004058255A1

  公开（公告）日：2004-07-15

  The present invention relates to compounds of formula (I): in which R1 and R2 independently represent phenyl, thienyl or pyridyl and R3 represents a group -X-Y-NR4R5 in which X is CO or SO2; Y is absent or represents NH and the other substituente are as defined in the description and their use in the treatment of obesity, psychiatric and neurological disorders and to pharmaceutical compositions containing them.

  本发明涉及以下式(I)的化合物：其中R1和R2分别表示苯基、噻吩基或吡啶基，R3表示一个基团-X-Y-NR4R5，其中X为CO或SO2；Y为不存在或表示NH，其他取代基如描述中所定义，并且它们在治疗肥胖、精神疾病和神经系统疾病以及含有它们的药物组合物中的应用。
• [EN] AQUEOUS DISPERSION COMPRISING STABLE NANOPARTICLES OF A WATER-INSOLUBLE THIAZOLE DERIVATIVE AND EXCIPIENTS LIKE MIDDLE CHAIN TRIGLYCERIDES<br/>[FR] DISPERSION AQUEUSE COMPRENANT DES NANOPARTICULES STABLES D'UN DERIVE DE THIAZOLE INSOLUBLE DANS L'EAU ET DES EXCIPIENTS TELS QUE DES TRIGLYCERIDES A CHAINE MOYENNE
  申请人：ASTRAZENECA AB

  公开号：WO2004069226A1

  公开（公告）日：2004-08-19

  A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a thiazole compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions obtainable by the process, solid particles obtainable by the process and use of such particles. The process provides a dispersion of solid particles in an aqueous medium, which particles exhibit reduced or substantially no particle growth mediated by Ostwald ripening. The process is particlularly suitable for the preparation of small (sub-micron) aqueous dispersions of a substantially water-insoluble pharmacologically active substance.

  一种制备固体颗粒稳定分散液的方法，其中该液体是在水介质中混合（a）第一个溶液，该溶液包括一种公式I的噻唑化合物，它是一种基本上不溶于水的物质，还包括一种水溶性有机溶剂和一种抑制剂，以及（b）一种水相，其中包括水和可选的稳定剂，从而沉淀出包含抑制剂和基本上不溶于水的物质的固体颗粒；可选地去除水溶性有机溶剂；其中抑制剂是根据描述定义的非聚合疏水有机化合物。还声明了通过该过程获得的稳定分散液，通过该过程获得的固体颗粒以及使用这种颗粒。该过程提供了一种固体颗粒在水介质中的分散液，这些颗粒表现出通过奥斯特瓦尔德成核介导的减少或基本上没有颗粒生长。该过程特别适用于制备基本上不溶于水的药理活性物质的小（亚微米）水分散液。
• Aqueous dispersion comprising stable nanoparticles of a water-insoluble thiazole derivative and excipients like middle chain triglycerides
  申请人：Lindfors Lennart

  公开号：US20060141043A1

  公开（公告）日：2006-06-29

  A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance which is a thiazole compound of Formula I, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. Also claimed are stable dispersions prepared by the process, solid particles prepared by the process and use of such particles.

  一种制备固体颗粒在水介质中稳定分散的方法，包括将（a）第一溶液与（b）水相结合。第一溶液包括具有公式I的噻唑化合物、水亲和性有机溶剂和抑制剂，该抑制剂为非聚合疏水性有机化合物。水相包括水和稳定剂，从而沉淀出包括抑制剂和基本上不溶于水的物质的固体颗粒；可选择去除水亲和性有机溶剂。还声明了由该方法制备的稳定分散液、由该方法制备的固体颗粒以及使用这些颗粒的用途。
• 4,5-diarylthiazole derivatives as cb-1 ligands
  申请人：Berggren Ingrid Kristina Anna

  公开号：US20060122229A1

  公开（公告）日：2006-06-08

  The present invention relates to compounds of formula (I): in which R 1 and R 2 independently represent phenyl, thienyl or pyridyl and R 3 represents a group —X—Y—NR 4 R 5 in which X is CO or SO 2 ; Y is absent or represents NH and the other substituente are as defined in the description and their use in the treatment of obesity, psychiatric and neurological disorders and to pharmaceutical compositions containing them.

  本发明涉及式(I)的化合物： 其中，R1和R2分别独立表示苯基、噻吩基或吡啶基，R3表示一个基团—X—Y—NR4R5，其中X为CO或SO2；Y为不存在或表示NH，其他取代基如描述所定义，并且它们在治疗肥胖症、精神和神经疾病以及含有它们的制药组合物中的应用。
• 4,5-DIARYLTHIAZOLE DERIVATIVES AS CB-1 LIGANDS
  申请人：AstraZeneca AB

  公开号：EP1581214A1

  公开（公告）日：2005-10-05